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My CartCAS：78415-72-2
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：White to off-white Solid
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| CAS | 78415-72-2 |
| Name | Milrinone |
| Molecular Formula | C12H9N3O |
| Molecular Weight | 211.22 |
| Solubility | Soluble in DMSO |
| Purity | HPLC≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 278-903-6 |
| MDL | MFCD00133539 |
| SMILES | CC(N1)=C(C2=CC=NC=C2)C=C(C#N)C1=O |
| InChIKey | PZRHRDRVRGEVNW-UHFFFAOYSA-N |
| InChI | InChI=1S/C12H9N3O/c1-8-11(9-2-4-14-5-3-9)6-10(7-13)12(16)15-8/h2-6H,1H3,(H,15,16) |
| PubChem CID | 4197 |
| Target Point | Phosphodiesterase (PDE) |
| Passage | Metabolic Enzyme&Protease |
| Background | Milrinone is a PDE3 inhibitor. |
| Biological Activity | Milrinone 是 PDE3 抑制剂，也是一种强心药、血管舒张药。[1-4] |
| In Vitro | 米力农(1μM)使缺氧肌细胞中的PKA活性增加至含氧量正常水平。米力农(50 nM)通过恢复PKA介导的调节性TP受体磷酸化来使缺氧心肌细胞中的TP受体敏感性正常化[1]。米力农显著降低NE诱导的血管收缩，减弱NE敏感性和最大张力产生。 ATP敏感性K +通道或电压门控K +通道的抑制不能阻止米力农诱导的NE反应衰减[4]。 |
| In Vivo | 米力农(1μg/ kg/min，iv)显著降低充血性心力衰竭(CHF)大鼠的PAP，PVR(-18.96±1.7％)和LAP(-26.03±2.3％)。米力农(1mg/mL，吸入)导致PAP的几乎最大降低而对AP没有显著影响，类似地在更大的CHF大鼠集体中降低肺动脉压。米力农吸入选择性地增加两组中的cAMP但不增加cGMP血浆浓度。重复吸入米力农甚至可降低肺湿/干重比[2]。米力农(49.5μg)在很大程度上使ESPVR向上移动并显著增加收缩末期压力(ESP(0.08))和中等LV容积(0.08 mL/g心肌)的收缩压 - 体积面积(PVA(0.08))。米力农还略微降低LV ESP(ESV)并降低Ea [3]。 |
| Animal Experiment | 在100±8g体重(bw)的幼年大鼠中，通过冠状动脉上主动脉条带诱导CHF。简言之，通过腹膜内注射氯胺酮(87mg/kg体重)和甲苯噻嗪(13mg/kg体重)麻醉大鼠。将大鼠置于仰卧位，剃去胸壁，并在通气期间用100％O 2在第三肋间进行左胸廓切开术。升主动脉从结缔组织中脱离，并通过植入具有0.8mm的限定内径的钛夹而部分闭塞。在手术闭合胸腔后，允许大鼠从麻醉中恢复。对于术后镇痛，大鼠在手术后和术后第一天肌肉注射250mg/kg体重的安乃近。假手术大鼠作为对照。从麻醉中恢复后，将动物置于笼中，自由饮水和标准实验室饮食。对于吸入，使用超声雾化器雾化米力农(0.2-5mg/mL)或NaCl(0.9％)，并在整个实验中使用的相同峰值吸气压力下吸入3分钟。如通过微量重量测定所确定的，1mg/mL米力农的3分钟雾化导致14μg磷酸二酯酶-3抑制剂的蒸发。因此，39μg/ kg的相应剂量与人类研究中的吸入剂量类似。对于静脉输送，米力农(初始推注量为2-10μg/ kg，然后是0.2-1μg/ kg/min)或等量的NaCl(0.9％;初始推注量为1.6 mL/kg，然后是10μL/ kg)/h)通过输液泵给药10分钟。 |
| Data Literature Source | [1]. Santhosh KT，et al. Milrinone attenuates thromboxane receptor-mediated hyperresponsiveness in hypoxic pulmonary arterial myocytes. Br J Pharmacol. 2011 Jul;163(6):1223-36. [2]. Hentschel T，et al. Inhalation of the phosphodiesterase-3 inhibitor milrinone attenuates pulmonary hypertension in a rat model of congestive heart failure. Anesthesiology. 2007 Jan;106(1):124-31. [3]. Kishi T，et al. Effects of milrinone on left ventricular end-systolic pressure-volume relationship of rat hearts in situ. Clin Exp Pharmacol Physiol. 2001 Sep;28(9):737-42. [4]. Taylor MS，et al. Effect of milrinone on small mesenteric artery vasoconstriction: role of K(+) channels. Am J Physiol. 1999 Jul;277(1 Pt 1):G69-78 |
| Unit | Bottle |
| Specification | 10mg 10mM*1mL in DMSO 50mg |
Milrinone 是 PDE3 抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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